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贝曲西班 /Betrixaban {[allProObj[0].p_purity_real_show]}

货号：A463156 同义名： PRT054021;MK-4448

Betrixaban is a highly potent, selective, and orally efficacious factor Xa inhibitor with IC50 of 1.2 nM (inhibition of Factor 10a).

Betrixaban 化学结构 CAS号：330942-05-7
Betrixaban 化学结构
CAS号：330942-05-7
Betrixaban 3D分子结构
CAS号：330942-05-7
Betrixaban 化学结构 CAS号：330942-05-7
Betrixaban 3D分子结构 CAS号：330942-05-7
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Betrixaban 纯度/质量文件 产品仅供科研

货号：A463156 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 Factor Xa ↓ 其他靶点 纯度
Rivaroxaban ++

Factor Xa, IC50: 0.7 nM

 		98%
Apixaban ++++

Factor Xa (human), Ki: 0.08 nM

Factor Xa (rabbit), Ki: 0.17 nM

 		98%
Edoxaban tosylate monohydrate +++

Factor Xa, Ki: 0.561 nM

 		98+%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Betrixaban 生物活性

描述 Serine protease factor Xa (fXa), positioned at the juncture of the intrinsic and the extrinsic pathways, play a pivotal role in the blood coagulation cascade [3]. Betrixaban is a highly potent, selective, and orally efficacious fXa inhibitor with IC50of 1.5 nM. In patch clamp hERG (human ether-a-go-go related gene) assays, Betrixaban has IC50 value of 8.9 μM. The plasma kallikrein IC50 and Ki values for Betrixaban are 6.3 μM and 3.5 μM respectively. Betrixaban (hERG Ki 1.8 μM) exhibits significantly lower hERG activity than all the others (hERG Ki⩽0.5 μM) [3]. Dosed at 0.5 mg/kg IV and 2.5 mg/kg PO, Betrixaban has bioavailability of 51.6% in dog; dosed at 0.75 mg/kg IV and 7.5 mg/kg PO, Betrixaban has bioavailability of 58.7% in monkey [3]. After i.v. infusion for 30 min, the total plasma concentration of Betrixaban is 0.2±0.01 μM, and the percentage of unbound inhibitor is 40%±7.2% [4].
作用机制 The chloropyridine A ring extents into the fXa S1 site with the chloro atom positioned above the phenyl ring of Tyr228 and occupies a hydrophobic pocket formed by Ala190, Val213 and Tyr228.

Betrixaban 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03728166 Venous Thromboembolism Phase 4 Not yet recruiting February 1, 2021 -
NCT03397888 Hepatic Impairment Phase 1 Completed - United States, Florida ... 展开 >> Clinical Pharmacology of Miami Hialeah, Florida, United States, 33014 收起 <<
NCT03613402 - Suspended(Due to slow enrollme... 展开 >>nt.) 收起 << January 2020 United States, North Carolina ... 展开 >> Durham Durham, North Carolina, United States, 27705 收起 <<

Betrixaban 参考文献

[1]Lu G, DeGuzman FR, et al. A specific antidote for reversal of anticoagulation by direct and indirect inhibitors of coagulation factor Xa. Nat Med. 2013 Apr;19(4):446-51.

[2]Zhang P, Huang W, et al. Discovery of betrixaban (PRT054021), N-(5-chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido)-5-methoxybenz amide, a highly potent, selective, and orally efficacious factor Xa inhibitor. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2179-85.

[3]Zhang P, Huang W, Wang L, Bao L, Jia ZJ, Bauer SM, Goldman EA, Probst GD, Song Y, Su T, Fan J, Wu Y, Li W, Woolfrey J, Sinha U, Wong PW, Edwards ST, Arfsten AE, Clizbe LA, Kanter J, Pandey A, Park G, Hutchaleelaha A, Lambing JL, Hollenbach SJ, Scarborough RM, Zhu BY. Discovery of betrixaban (PRT054021), N-(5-chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido)-5-methoxybenzamide, a highly potent, selective, and orally efficacious factor Xa inhibitor. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2179-85. doi: 10.1016/j.bmcl.2009.02.111. Epub 2009 Mar 3. PMID: 19297154.

[4]Lu G, DeGuzman FR, Hollenbach SJ, Karbarz MJ, Abe K, Lee G, Luan P, Hutchaleelaha A, Inagaki M, Conley PB, Phillips DR, Sinha U. A specific antidote for reversal of anticoagulation by direct and indirect inhibitors of coagulation factor Xa. Nat Med. 2013 Apr;19(4):446-51. doi: 10.1038/nm.3102. Epub 2013 Mar 3. PMID: 23455714.

Betrixaban 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.21mL

0.44mL

0.22mL

11.06mL

2.21mL

1.11mL

22.13mL

4.43mL

2.21mL

Betrixaban 技术信息

CAS号330942-05-7
分子式C23H22ClN5O3
分子量 451.906
别名 PRT054021;MK-4448;MLN1021
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C
溶解度

DMSO: 25 mg/mL(55.32 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

Tags: Betrixaban | 330942-05-7 | PRT054021 | PRT 054021 | PRT-054021 | Factor Xa Inhibitor | Metabolic Enzyme/Protease | Factor Xa | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Betrixaban 纯度/质量文件 | Betrixaban 亚型比较 | Betrixaban 生物活性 | Betrixaban 临床数据 | Betrixaban 参考文献 | Betrixaban 实验方案 | Betrixaban 技术信息

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